A new series of 2-aralkynyl-N6-methyl-MECAs 10-13 were synthesized and evaluated in radioligand binding studies and in a newEu-GTP functional assay that provides a powerful alternative to radioisotope use. The new compounds possess high affinity and selectivity for the AA3R with N6-methyl-2-phenylethynylMECA (10) showing a subnanomolar affinity and about 100000-fold selectivity vs AA1R and AA2AR. Furthermore, the new nucleosides showed to be full agonists, the N 6-methyl-2-(2-pyridinyl)-ethynylMECA (13) being the most potent in the series.
Synthesis and biological evaluation of 2-alkynyl-N6-methyl-5'-N-methylcarboxamidoadenosine derivatives as potent and highly selective agonists for the human adenosine A3 receptor / R. Volpini, M. Buccioni, D. Dal Ben, C. Lambertucci, C. Lammi, G. Marucci, A.T. Ramadori, K. Klotz, G. Cristalli. - In: JOURNAL OF MEDICINAL CHEMISTRY. - ISSN 0022-2623. - 52:23(2009 Dec 10), pp. 7897-7900.
Synthesis and biological evaluation of 2-alkynyl-N6-methyl-5'-N-methylcarboxamidoadenosine derivatives as potent and highly selective agonists for the human adenosine A3 receptor
C. Lammi;
2009
Abstract
A new series of 2-aralkynyl-N6-methyl-MECAs 10-13 were synthesized and evaluated in radioligand binding studies and in a newEu-GTP functional assay that provides a powerful alternative to radioisotope use. The new compounds possess high affinity and selectivity for the AA3R with N6-methyl-2-phenylethynylMECA (10) showing a subnanomolar affinity and about 100000-fold selectivity vs AA1R and AA2AR. Furthermore, the new nucleosides showed to be full agonists, the N 6-methyl-2-(2-pyridinyl)-ethynylMECA (13) being the most potent in the series.
Pubblicazioni consigliate
I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
